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Signal Pathway


In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.

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    SP600125是一种广谱JNK抑制剂,作用于JNK1, JNK2和JNK3时,IC50分别为40 nM, 40 nM和90 nM,比作用于MKK4选择性高10倍,比作用于MKK3, MKK6, PKB,和PKCα选择性高25倍,比作用于ERK2, p38, Chk1, EGFR等选择性高100倍。

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    Ibrutinib (PCI-32765)是一种有效的,高选择性的Btk抑制剂,IC50为0.5 nM,能稍许微抑制Bmx, CSK, FGR, BRK及HCK,但对EGFR, Yes, ErbB2, JAK3等作用效果稍弱。

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    Fludarabine, a purine analog, is used in the treatment of hematological malignancies for the inhibition of STAT-1 activation and DNA synthesis. Fludarabine是一种STAT1活性抑制剂和DNA合成抑制剂。

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    TNF-α inhibitor Lenalidomide (CC-5013, LEN) is an immunomodulatory drug currently approved for the treatment of multiple myeloma (MM), 5q- myelodysplasia and mantle cell lymphoma. Lenalidomide (CC-5013)是Thalidomide的衍生物,是一种TNF-α分泌抑制剂,IC50为13 nM。

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